词条 | ERB-196 |
释义 |
| Verifiedfields = | Watchedfields = | verifiedrevid = | IUPAC_name = 3-(3-Fluoro-4-hydroxyphenyl)-7-hydroxynaphthalene-1-carbonitrile | image = ERB-196.svg | width = 250px | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = | CAS_number = 550997-55-2 | CAS_supplemental = | ATC_prefix = | ATC_suffix = | ATC_supplemental = | PubChem = 6102691 | IUPHAR_ligand = | DrugBank_Ref = | DrugBank = DB06875 | ChemSpiderID_Ref = | ChemSpiderID = 4810213 | UNII = | KEGG = | ChEBI = | ChEMBL = 192154 | synonyms = WAY-202196 | C=17 | H=10 | F=1 | N=1 | O=2 | molecular_weight = 279.27 g/mol | SMILES = C1(=CC2=C(C(=C1)C#N)C=C(C=C2)O)C1=CC(=C(C=C1)O)F | StdInChI_Ref = | StdInChI = 1S/C17H10FNO2/c18-16-7-10(2-4-17(16)21)12-5-11-1-3-14(20)8-15(11)13(6-12)9-19/h1-8,20-21H | StdInChIKey_Ref = | StdInChIKey = NSSOSHDCWCMNDM-UHFFFAOYSA-N }}ERB-196, also known as WAY-202196, is a synthetic nonsteroidal estrogen that acts as a highly selective agonist of the ERβ.[1][2][3][4][5][6] It possesses 78-fold selectivity for the ERβ over the ERα.[1] The drug was under development by Wyeth for the treatment of inflammation and sepsis starting in 2004 but development was discontinued by 2011.[2][7] See also
References1. ^1 {{cite book|author=R. E. Hubbard|title=Structure-based Drug Discovery: An Overview|url=https://books.google.com/books?id=Q_Kj1Qvgob4C&pg=PA241|year=2006|publisher=Royal Society of Chemistry|isbn=978-0-85404-351-4|pages=241–}} 2. ^1 https://adisinsight.springer.com/drugs/800021229{{dead link|date=December 2016 |bot=InternetArchiveBot |fix-attempted=yes }} 3. ^{{cite book|title=Estrogens—Advances in Research and Application: 2013 Edition: ScholarlyBrief|url=https://books.google.com/books?id=NYW4rG83zrUC&pg=PA52|date=21 June 2013|publisher=ScholarlyEditions|isbn=978-1-4816-8771-3|pages=52–}} 4. ^{{cite book|author1=Eckhard Ottow|author2=Hilmar Weinmann|title=Nuclear Receptors as Drug Targets|url=https://books.google.com/books?id=iATfLbPgRugC&pg=PA66|date=8 September 2008|publisher=John Wiley & Sons|isbn=978-3-527-62330-3|pages=66–}} 5. ^{{cite journal | vauthors = Mewshaw RE, Edsall RJ, Yang C, Manas ES, Xu ZB, Henderson RA, Keith JC, Harris HA | title = ERbeta ligands. 3. Exploiting two binding orientations of the 2-phenylnaphthalene scaffold to achieve ERbeta selectivity | journal = J. Med. Chem. | volume = 48 | issue = 12 | pages = 3953–79 | year = 2005 | pmid = 15943471 | doi = 10.1021/jm058173s | url = }} 6. ^{{cite journal | vauthors = Cristofaro PA, Opal SM, Palardy JE, Parejo NA, Jhung J, Keith JC, Harris HA | title = WAY-202196, a selective estrogen receptor-beta agonist, protects against death in experimental septic shock | journal = Crit. Care Med. | volume = 34 | issue = 8 | pages = 2188–93 | year = 2006 | pmid = 16755255 | doi = 10.1097/01.CCM.0000227173.13497.56 | url = }} 7. ^{{cite book|author=Jean-Louis Vincent|title=Yearbook of Intensive Care and Emergency Medicine 2007|url=https://books.google.com/books?id=zT8_AAAAQBAJ&pg=PA891|date=8 December 2007|publisher=Springer Science & Business Media|isbn=978-3-540-49433-1|pages=891–}} External links
6 : Phenols|Fluoroarenes|Naphthalenes|Nitriles|Selective ERβ agonists|Synthetic estrogens |
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